Cancer has become the first threat to human health. Chemotherapy is the major means for treating neoplastic diseases. While the nausea and emesis is one of the most common side effects from anti-cancer chemotherapy. Severe emesis can lead to dehydration, electrolyte imbalance, weakness, and even the patient refused treatment. Currently the main use of antiemetic granisetron is 5-HT3 antagonist.
Palonosetron has recently emerged as a highly efficacious anti-nauseant and anti-emetic during anti-cancer chemotherapy. Palonosetron is selective, showing a high affinity as an antagonist for the 5-hydroxyltry ptamine 3 receptor precursor (5-HT3 receptor), and has the advantage of high efficacy, long duration, tolerability and fewer side-effect when compared with the traditional 5-HT3 receptors.
Palonosetron is sold as a sterile injectable liquid in the United States in July 2003 as ALOXI® by MGI Pharma and Helsinn Healthcare SA. After listing, it soon became the first choice for prevention of nausea and vomiting. At present, the listed products also have capsules and sprays. Despite numerous clinical benefits and advantages of this intravenous formulation, it is generally recognized that injection drug delivery systems present special problems with respect to storage life and stability of the active agent. Injection is also inconvenient when self-administered, and has an increased risk of contamination and human error. Oral administration may induce patient nausea, which resulting in vomiting out chemotherapeutic agents and reducing the efficacy of the chemotherapeutic agent. Further, some patients cannot use capsules due to difficulty swallowing.
There exists a need for a method and a composition for delivering palonosetron with improved bioavailability and fewer side effects.